公开(公告)号：US20040266780A1

公开(公告)日：2004-12-30

申请号：US10697912

申请日：2003-10-30

发明人： Chanchal Sadhu ,  Ken Dick ,  Jennifer Treiberg ,  C. Gregory Sowell ,  Edward A. Kesicki ,  Amy Oliver

IPC分类号： A61K031/497 ,  A61K031/501 ,  A61K031/506 ,  A61K031/4709

CPC分类号： A61K31/506 ,  C07D403/12 ,  C07D473/00 ,  C07D473/16 ,  C07D473/24 ,  C07D473/30 ,  C07D473/32 ,  C07D473/34 ,  C07D473/38 ,  C07D473/40 ,  C07D487/04 ,  C12N9/1205 ,  C12N9/99 ,  C12Y207/01137

摘要： Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Knull) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Knull plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Knull, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Knull activity, including compounds that selectively inhibit PI3Knull activity. Methods of using PI3Knull inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Knull inhibitory compounds to inhibit PI3Knull-mediated processes in vitro and in vivo.

摘要翻译： 公开了抑制磷脂酰肌醇3-激酶δ同种型（PI3Kdelta）活性的方法，以及治疗PI3Kdelta在白细胞功能中起作用的疾病如免疫和炎症疾病的方法。 优选地，所述方法使用选择性抑制PI3Kdelta的活性剂，而不显着抑制其它PI3K同种型的活性。 提供抑制PI3Kdelta活性的化合物，包括选择性抑制PI3Kdelta活性的化合物。 还提供了使用PI3Kdelta抑制化合物抑制癌细胞生长或增殖的方法。 因此，本发明提供了使用PI3Kdelta抑制化合物在体外和体内抑制PI3Kdelta介导的过程的方法。

公开(公告)号：US20040259886A1

公开(公告)日：2004-12-23

申请号：US10840577

申请日：2004-05-06

申请人： Pfizer Inc

发明人： Wesley W. Day ,  Andrew G. Lee ,  David D. Thompson

IPC分类号： A61K031/517 ,  A61K031/506 ,  A61K031/401

CPC分类号： A61K45/06 ,  A61K31/40 ,  A61K31/565 ,  A61K2300/00

摘要： This invention relates to methods, pharmaceutical compositions and kits useful in promoting bone formation and/or preventing bone loss and lowering blood cholesterol. The compositions are comprised of an estrogen agonist/antagonist as a first active component and a statin as a second active component and a pharmaceutically acceptable vehicle, carrier or diluent. The compositions and methods of treatment are effective while substantially reducing the concomitant liability of adverse effects associated with estrogen administration.

公开(公告)号：US20040242613A1

公开(公告)日：2004-12-02

申请号：US10766079

申请日：2004-01-27

申请人： Boehringer Ingelheim Pharmaceuticals, Inc. ,  Boehringer Ingelheim Pharma GmbH & Co. KG

发明人： Mario G. Cardozo ,  Derek Cogan ,  Charles Lawrence Cywin ,  Georg Dahmann ,  Darren DiSalvo ,  John David Ginn ,  Anthony S. Prokopowicz III ,  Denice M. Spero ,  Erick Young

IPC分类号： A61K031/506 ,  A61K031/505

CPC分类号： C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04 ,  H01L51/0089

摘要： Disclosed are novel compounds of formula (I): 1 wherein R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

摘要翻译： 公开了式（I）的新化合物：其中R 1，R 2和R 3如本文所定义，其可用作PKC-θ的抑制剂，因此可用于治疗通过该活性介导或维持的多种疾病和病症 的PKC-θ，包括免疫学障碍和II型糖尿病。 本发明还涉及包含这些化合物的药物组合物，使用这些化合物治疗各种疾病和病症的方法，制备这些化合物的方法和可用于这些方法的中间体。

公开(公告)号：US20040242578A1

公开(公告)日：2004-12-02

申请号：US10451305

申请日：2004-06-09

发明人： Amogh Boloor ,  Mui Cheung ,  Ronda Davis ,  Philip Amthony Harris ,  Kevin Hinkle ,  Robert Anthony Mook JR. ,  Jeffrey Alan Stafford ,  James Marvin Veal

IPC分类号： A61K031/53 ,  A61K031/506 ,  C07D43/02

CPC分类号： C07D239/30 ,  C07D231/56 ,  C07D235/08 ,  C07D403/12 ,  C07D413/14

摘要： Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.

摘要翻译： 本文描述了可用作VEGFR2抑制剂的嘧啶衍生物。 所述的发明还包括制备此类嘧啶衍生物的方法以及使用该嘧啶衍生物的方法来治疗过度增殖性疾病。

公开(公告)号：US20040235834A1

公开(公告)日：2004-11-25

申请号：US10809944

申请日：2004-03-25

发明人： Luc J. Farmer ,  Edmund Martin Harrington ,  Francesco G. Salituro ,  Jian Wang

IPC分类号： A61K031/541 ,  A61K031/5377 ,  A61K031/506 ,  C07D417/14

CPC分类号： C07D417/14 ,  C07D417/04

摘要： The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

摘要翻译： 本发明涉及可用于蛋白激酶抑制剂的化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。

公开(公告)号：US20040224944A1

公开(公告)日：2004-11-11

申请号：US10624800

申请日：2003-07-22

发明人： David Bebbington ,  Hayley Binch ,  Ronald Knegtel ,  Julian Golec ,  Sanjay Patel ,  Jean-Damien Charrier ,  David Kay ,  Robert Davies ,  Pan Li ,  Marion Wannamaker ,  Cornelia Forster ,  Albert Pierce

IPC分类号： A61K031/541 ,  A61K031/5377 ,  A61K031/506 ,  C07D43/14 ,  C07D413/14 ,  C07D417/14

CPC分类号： C07D401/14 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/16 ,  C07D487/04 ,  C07D491/04 ,  C07D491/10 ,  C07D493/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

摘要： This invention describes novel pyrazole compounds of formula IV: 1 wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R2, R2null, T, and R3 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

摘要翻译： 本发明描述了式IV的新型吡唑化合物：其中环D是5-7元单环或选自芳基，杂芳基，杂环基或碳环基的8-10元双环; R x和R y独立地选自TR 3，或者与它们的插入原子一起形成具有1-3个选自氧，C 1 -C 6烷基的环杂原子的稠合，不饱和或部分不饱和的5-8元环， 硫或氮; R 2，R 2'，T和R 3如说明书中所述。 这些化合物可用作蛋白激酶抑制剂，特别是作为用于治疗诸如癌症，糖尿病和阿尔茨海默病的疾病的极光-2和GSK-3的抑制剂。

公开(公告)号：US20040220177A1

公开(公告)日：2004-11-04

申请号：US10734039

申请日：2003-12-11

申请人： Pfizer Inc

发明人： John Charles Kath ,  Michael Joseph Luzzio

IPC分类号： A61K031/55 ,  A61K031/513 ,  A61K031/506 ,  C07D43/02

CPC分类号： C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D513/04

摘要： The invention relates to compounds of the formula 1 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3, R4, R5, n, A and B are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.

摘要翻译： 本发明涉及式1的化合物及其药学上可接受的盐，前药和溶剂合物，其中R 1，R 2，R 3，R 4，R 5，n，A和 B如本文所定义。 本发明还涉及通过施用式1的化合物和用于治疗这些疾病的药物组合物来治疗哺乳动物异常细胞生长的方法，其含有式1的化合物。本发明还涉及制备式1化合物的方法 。

公开(公告)号：US20040213843A1

公开(公告)日：2004-10-28

申请号：US10852733

申请日：2004-05-24

发明人： J. G. J. Egberink ,  J. F. Engelhart

IPC分类号： A61K031/506 ,  A61K009/20

CPC分类号： A61K9/2054

摘要： This invention makes a pharmaceutical formulation for oral administration with extended release properties available comprising an amount of gepirone hydrochloride, an amount of a cellulosic polymer matrix and an amount of microcrystalline cellulose characterised in that the amount the pharmaceutically acceptable cellulosic polymer matrix is from 70 to 85 wt %, the amount of carbohydrate binder is from 7 to 10 wt % and the amount of gepirone hydrochloride is from 13 to 21 wt %. The formulation is useful for a treatment for depression or a related central nervous system disorder with gepirone administered in a once-a-day oral formulation for extended release of gepirone.

摘要翻译： 本发明制备用于具有延长释放性质的口服给药的药物制剂，其包含一定量的盐酸吉哌隆，纤维素聚合物基质的量和微晶纤维素的量，其特征在于药学上可接受的纤维素聚合物基质的量为70至85 重量％，碳水化合物粘合剂的量为7〜10重量％，盐酸吉比隆的含量为13〜21重量％。 该制剂可用于治疗抑郁症或相关的中枢神经系统疾病，其中使用吉哌隆以每天一次口服制剂延长释放吉非隆。

公开(公告)号：US20040198739A1

公开(公告)日：2004-10-07

申请号：US10485636

申请日：2004-02-03

发明人： Jerome Emile Georges Guillemont ,  Patrice Palandjian ,  Marc Rene de Jonge ,  Lucien Maria Henricus Koymans ,  Hendrik Maarten Vinkers ,  Frederik Frans Desire Daeyaert ,  Jan Heeres ,  Koen Jeanne Alfons Van Aken ,  Paulus Joannes Lewi ,  Paul Adriaan Jan Janssen

IPC分类号： A61K031/506 ,  A61K031/501 ,  C07D43/14

CPC分类号： C07D239/48 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07C255/42 ,  C07C257/12 ,  C07D239/47 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： This invention concerns HIV replication inhibitors of formula (I) the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a1nulla2-a3nulla4- and -b1nullb2-b3nullb4- represents pheynl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl;n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl, substituted C1-6alkyl, C1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, nullS(nullO)pR6, nullNHnullS(nullO)pR6, nullC(nullO)R6, nullNHC(nullO)H, nullC(nullO)NHNHnull2null, nullNHC(nullO)R6, nullC(nullNH)R6 or a 5-membered hetrocycl; X1 is nullNR5null, nullNHnullNHnull, nullNnullNnull, nullOnull, nullC(nullO)null, C1-4alkanediyl, nullCHOHnull, nullSnull, nullS(nullO)pnull, nullX2nullC1-4alkanediyl- or nullC1-4alkanediyl-X2null; R3 is NHR13, NR13R14; nullC(nullO)nullNHR13; nullC(nullO)nullNR13R14; nullC(nullO)nullR15; nullCHnullNnullNHnullC(nullO)nullR16; substituted C1-6alkyl; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl; substituted C2-6alkynyl; substituted C2-6alkylenyl; C1-6alkyl substituted with hydroxy and a second substituent; nullC(nullNnullOnullR8)nullC1-4alkyl; R7; or nullX3nullR7; R4 is halo, hydroxy, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxy, cyano, nitro, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyl, formyl, amino, mono- or di(C1-4alkyl) amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them. 1

摘要翻译： 本发明涉及式（I）的N-复合抑制剂，其N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式，其中含-a 1 = a 2 -a 3 n = 0〜5; b 1 = b 2 -b 3 = b 4 - 表示吡啶基，吡啶基，嘧啶基，吡嗪基，哒嗪基; n为0〜5; m为1〜4; R 1是氢; 芳基; 甲酰基 C 1-6烷基羰基; C 1-6烷基; C 1-6烷氧基羰基，取代的C 1-6烷基，C 1-6烷基羰基; R 2是羟基，卤素，任选取代的C 1-6烷基，C 3-7环烷基，任选取代的C 2-6烯基，任选取代的C 2-6炔基，C 1-6烷氧基，C 1-6烷氧基羰基，羧基，氰基，硝基，氨基，单或 （C 1-6烷基）氨基，多卤甲基，多卤代甲氧基，多卤甲硫基，-S（= O）pR 6，-NH-S（= O）p R 6，-C（= O）R 6， NHC（= O）H，-C（= O）NHNH 2，-NHC（= O）R 6，-C（= NH）R 6或5元环庚烯; X1是-NR5 - ， - NH-NH-，-N = N-，-O - ， - C（= O） - ，C1-4烷二基，-CHOH-，-S-，-S（= O ）p-，-X2-C1-4烷二基或-C1-4烷二基X2-; R 3是NHR 13，NR 13 R 14; -C（= O）-NHR 13; -C（= O）-NR 13 R 14; -C（= O）-R 15; -CH = N-NH-C（= O）-R 16; 取代的C 1-6烷基; 任选取代的C 1-6烷氧基C 1-6烷基; 取代的C 2-6烯基; 取代的C 2-6炔基; 取代的C2-6亚烷基; C

公开(公告)号：US20040192730A1

公开(公告)日：2004-09-30

申请号：US10799490

申请日：2004-03-12

申请人： Dynogen Pharmaceuticals, Inc.

发明人： Karl Bruce Thor

IPC分类号： A61K031/4545 ,  A61K031/506 ,  A61K031/501

CPC分类号： A61K31/437 ,  A61K31/40 ,  A61K31/404 ,  A61K31/4245 ,  A61K31/4365 ,  A61K31/4545 ,  A61K31/46 ,  A61K31/496 ,  A61K31/538

摘要： A method is provided for using compounds that exhibit combined activities as 5-HT1A active agents and selective serotonin reuptake inhibitors (SSRI's) to treat sexual dysfunction, particularly premature ejaculation, on an as-needed basis shortly before sexual activity.

摘要翻译： 提供了一种使用化合物作为5-HT1A活性剂和选择性5-羟色胺再摄取抑制剂（SSRI's）的化合物在性活动前不久就根据需要治疗性功能障碍，特别是早泄的方法。